Vemurafenib: the first drug approved for BRAF-mutant cancer

G Bollag, J Tsai, J Zhang, C Zhang, P Ibrahim… - Nature reviews Drug …, 2012 - nature.com
The identification of driver oncogenes has provided important targets for drugs that can
change the landscape of cancer therapies. One such example is the BRAF oncogene, which …

Vemurafenib

KT Flaherty, U Yasothan, P Kirkpatrick - Nature reviews Drug discovery, 2011 - go.gale.com
In August 2011 vemurafenib (Zelboraf; Daiichi Sankyo/Roche), an inhibitor of BRAF kinase,
was approved by the US Food and Drug Administration (FDA) for the treatment of patients …

Pan-Cancer Efficacy of Vemurafenib in BRAFV600-Mutant Non-Melanoma Cancers

V Subbiah, I Puzanov, JY Blay, I Chau, AC Lockhart… - Cancer discovery, 2020 - AACR
BRAF V600 mutations occur in a wide range of tumor types, and RAF inhibition has become
standard in several of these cancers. Despite this progress, BRAF V600 mutations have …

BRAF targeted therapy changes the treatment paradigm in melanoma

A Ribas, KT Flaherty - Nature reviews Clinical oncology, 2011 - nature.com
After decades of stagnation, recent therapeutic advances in melanoma seem on the horizon.
The discovery of the genetic underpinnings of this historically refractory disease has …

Targeting mutant BRAF in melanoma: current status and future development of combination therapy strategies

R Kudchadkar, KHT Paraiso, KSM Smalley - The Cancer Journal, 2012 - journals.lww.com
The discovery of activating BRAF mutations in∼ 50% of all melanomas has proved to be a
turning point in the therapeutic management of the disseminated disease. In this …

BRAF mutations: signaling, epidemiology, and clinical experience in multiple malignancies

RD Hall, RR Kudchadkar - Cancer Control, 2014 - journals.sagepub.com
Background Mutations in BRAF were first reported in 2002. Since that time, the molecular
basis for oncogenic signaling has been elucidated in multiple malignancies. The …

Vemurafenib: Targeted Inhibition of Mutated BRAF for Treatment of Advanced Melanoma and Its Potential in Other Malignancies

A Sharma, SR Shah, H Illum, J Dowell - Drugs, 2012 - Springer
Vemurafenib is the first molecularly targeted therapy to be licensed in the US and Europe for
treatment of advanced melanoma. Its mechanism of action involves selective inhibition of the …

Emerging insights into resistance to BRAF inhibitors in melanoma

AD Bucheit, MA Davies - Biochemical pharmacology, 2014 - Elsevier
Melanoma is the most aggressive form of skin cancer. The treatment of patients with
advanced melanoma is rapidly evolving due to an improved understanding of molecular …

Analytical performance of a real-time PCR-based assay for V600 mutations in the BRAF gene, used as the companion diagnostic test for the novel BRAF inhibitor …

H Halait, K DeMartin, S Shah, S Soviero… - Diagnostic Molecular …, 2012 - journals.lww.com
Melanomas frequently harbor BRAFV600 mutations. Vemurafenib (RG7204/PLX4032), a
small-molecule inhibitor of mutant BRAF, has shown striking clinical efficacy in BRAFV600 …

BRAF inhibitors in cancer therapy

CH Johansson, SE Brage - Pharmacology & therapeutics, 2014 - Elsevier
Activating BRAF mutations, leading to constitutive activation of the MAPK signaling pathway,
are common in a variety of human cancers. Several small molecule BRAF inhibitors have …